| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Midodrine targets the α1-adrenergic receptor as a selective agonist. α1-adrenergic receptors are G protein-coupled receptors located on vascular smooth muscle cells. Activation of these receptors by midodrine's active metabolite leads to vasoconstriction, increased peripheral vascular resistance, and elevation of blood pressure. Midodrine is a prodrug of the α1-adrenergic receptor agonist, 1-(2',5'-dimethoxyphenyl)-2-aminoethanol. It is a direct-acting sympathomimetic drug with selective α-adrenergic agonist activity.
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| ln Vitro |
In vitro, midodrine hydrochloride is characterized as an α1-receptor agonist. The compound's active metabolite, desglymidodrine, binds to and activates α1-adrenergic receptors on vascular smooth muscle, leading to vasoconstriction. Midodrine's selectivity for α1 receptors over α2 receptors contributes to its vasopressor effects with minimal central nervous system stimulation. The compound's in vitro activity has been confirmed in receptor binding and functional assays.
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| ln Vivo |
In vivo, midodrine hydrochloride acts as a peripheral vasoconstrictor to treat hypotensive conditions. It is used clinically for the treatment of dysautonomia and orthostatic hypotension. The drug increases arterial pressure by activating α1-adrenergic receptors in the vasculature, producing an increase in vascular tone and elevation of blood pressure. Midodrine improves clinical outcomes in patients with chronic hypotension. It is administered orally and is well-absorbed.
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| Enzyme Assay |
In non-cell-based receptor binding assays, midodrine's affinity for the α1-adrenergic receptor is evaluated using radioligand competition binding experiments. Membrane preparations from cells expressing recombinant human α1-adrenergic receptors are incubated with a radiolabeled α1-selective ligand and varying concentrations of midodrine or its active metabolite. After incubation, bound and free radioligand are separated, and radioactivity is measured. Competition curves are generated to determine IC50 and Ki values, confirming the compound's α1-adrenergic receptor agonist activity.
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| Cell Assay |
In vitro cellular assays for midodrine involve measuring its agonist activity at the α1-adrenergic receptor in cultured cells. Cells expressing recombinant α1-adrenergic receptors are treated with midodrine or its active metabolite, and receptor activation is assessed by measuring downstream signaling pathways such as calcium mobilization or inositol phosphate accumulation. These functional assays confirm that midodrine's active metabolite acts as an α1-adrenergic receptor agonist.
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| Animal Protocol |
In vivo animal studies for midodrine have been conducted in models of hypotension. The compound is typically administered orally or intravenously, and its effects on blood pressure and vascular tone are measured. Midodrine's ability to increase arterial pressure has been demonstrated in animal models and clinical studies. Detailed protocols and data from specific animal models are limited in publicly available sources but are consistent with its clinical use as a vasopressor.
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| ADME/Pharmacokinetics |
Midodrine hydrochloride is well absorbed after oral administration and is converted to its active metabolite, desglymidodrine, which is responsible for its vasopressor effects. The drug has a relatively short half-life and is eliminated primarily by renal excretion. It is administered multiple times daily to maintain blood pressure control. The compound is soluble in DMSO at 53 mg/mL (182.29 mM). Storage conditions for the powder are -20°C for 3 years.
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| Toxicity/Toxicokinetics |
The most common side effects of midodrine include hypertension (particularly in the supine position), piloerection, urinary retention, and paresthesia. Because it increases blood pressure, it should be used with caution in patients with hypertension, heart failure, or renal impairment. The drug should be administered in a manner that minimizes the risk of supine hypertension. Midodrine should not be used in patients with severe organic heart disease, acute renal disease, or pheochromocytoma.
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| Additional Infomation |
Midodrine hydrochloride is a hydrochloride salt formed by the combination of equimolar amounts of midodrine and hydrogen chloride. Midodrine is a direct-acting sympathomimetic drug with selective α-adrenergic agonist activity. This hydrochloride salt is used as a peripheral vasoconstrictor to treat certain hypotensive conditions. Its main active ingredient is its major metabolite, desglycinedoryidodrine. Desglycinedoryidodrine has the effects of an α-adrenergic agonist, sympathomimetic drug, and vasoconstrictor. It contains midodrine (1+). Midodrine hydrochloride is the hydrochloride form of midodrine, a direct-acting prodrug and sympathomimetic drug with antihypertensive effects. Midodrine is converted to its active metabolite, desglycinedoryidodrine, via a deglycination reaction. Desglycinedoryidodrine selectively binds to and activates α1-adrenergic receptors in arterioles and venules. This leads to smooth muscle contraction, thereby increasing blood pressure. Desglycinedoryidodrine has difficulty crossing the blood-brain barrier and therefore does not affect the central nervous system. It is an ethanolamine derivative, belonging to the α1-adrenergic agonist class. It is used as a vasoconstrictor to treat hypotension. See also: Midordine (containing the active ingredient).
Midodrine hydrochloride is approved for the treatment of orthostatic hypotension and dysautonomia. It is available under various brand names including Amatine, Orvaten, and Pro-Amatine. Midodrine is a prodrug that is converted to its active metabolite, desglymidodrine, which acts as a selective α1-adrenergic receptor agonist. The drug's vasopressor effects are mediated through peripheral vasoconstriction, leading to increased blood pressure. It is a direct-acting sympathomimetic agent. |
| Molecular Formula |
C12H19CLN2O4
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|---|---|
| Molecular Weight |
290.74
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| Exact Mass |
290.103
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| CAS # |
43218-56-0
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| Related CAS # |
Midodrine-d6 hydrochloride;1188265-43-1;Midodrine;42794-76-3
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| PubChem CID |
18340
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| Appearance |
White to yellow solid powder
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| Boiling Point |
529.9ºC at 760 mmHg
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| Flash Point |
274.3ºC
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| LogP |
1.705
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
19
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| Complexity |
263
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MGCQZNBCJBRZDT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H18N2O4.ClH/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13;/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16);1H
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| Chemical Name |
2-Amino-N-(2-(2,5-dimethoxyphenyl)-2-hydroxyethyl)acetamide monohydrochloride
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| Synonyms |
Midodrine HCl Pro-Amatine Amatine OrvatenMidodrine hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~343.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4395 mL | 17.1975 mL | 34.3950 mL | |
| 5 mM | 0.6879 mL | 3.4395 mL | 6.8790 mL | |
| 10 mM | 0.3439 mL | 1.7197 mL | 3.4395 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| Completed | NCT03129542 | Drug: Midodrine Hydrochloride 10 milligrams
Drug: Placebo capsule |
Blood Pressure Sepsis |
Mayo Clinic | 2017-08-30 | Phase 1 |
| NCT00650013 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-07 | Phase 1 |
| NCT00648440 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-10 | Phase 1 |
| NCT00650364 | Completed | Drug: Midodrine HCl Tablets 5 mg Drug: ProAmatine® Tablets 5 mg |
Healthy | Mylan Pharmaceuticals Inc | 2002-08 | Phase 1 |
| Completed WITH RESULTS | NCT00426842 | Drug: Midodrine Hydrochloride | Orthostatic Hypotension Spinal Cord Injury |
James J. Peters Veterans Affairs Medical Center | 2007-01 | Phase 2 |
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